Abstract: A composition for the sequestration and sustained delivery of an active ingredient in the form of porous particles, the composition comprising the product of the controlled dehydration of particles formed by the reaction of a polymeric anionic material with a polyvalent cation. The composition may be loaded with an active ingredient by soaking the particles in a solution of the active ingredient; and may then be dehydrated. They may then be soaked in a solution of a polymeric cationic material, to form particles providing the controlled release of the active ingredient.

Abstract: Polymers useful as orthopedic implants or vehicles for the sustained delivery of pharmaceutical, cosmetic and agricultural agents are prepared in such a manner that the rate and degree to which they are hydrolyzed can be controlled without addition of exogenous acid. This control results from the incorporation of esters of short-chain .alpha.-hydroxy acids such as esters of glycolic acid, lactic acid or glycolic-co-lactic acid copolymer into the polymer chain and variation of the amount of these esters relative to the polymer as a whole.

Abstract: PEG-POE, PEG-POE-PEG, and POE-PEG-POE block copolymers have both hydrophilic and hydrophobic blocks. They form micelles in aqueous solution, making them suitable for encapsulation or solubilization of hydrophobic or water-insoluble materials; and they also form bioerodible matrices for the sustained release of active agents, especially when the POE block(s) contain at least one unit containing an .alpha.-hydroxy acid.

Abstract: Bioerodible ortho ester polymers useful for preparing bioerodible pharmaceutical compositions such as implants, ointments, creams, gels and the like are provided. The pharmaceutical compositions of the invention are useful for the controlled release of therapeutic agents, and may be administered for a variety of purposes, such as for the treatment of deep wounds, including burns, and for the treatment of periodontal disease.

Abstract: Bioerodible ortho ester polymers useful for preparing solid form bioerodible pharmaceutical compositions such as pellets, capsules, suppositories and the like are provided. A novel synthetic method for preparing the polymers is provided as well as is a novel triol reactant. Synthesis involves a one-step reaction between a monomeric ortho ester and a triol. The pharmaceutical compositions of the invention are useful for the controlled release of therapeutic agents, and may be administered for a variety of purposes.

Abstract: A composition for the transdermal delivery of a biologically active peptide having a molecular weight of about 5,000 or less comprising at lest one biologically active peptide, at least one higher alcohol, ester and/or higher amide in combination with at least one pyrrolidone compound of the formula: ##STR1## where R.sub.5 is hydrogen or a lower alkyl group having 1 to 4 carbon atoms, R.sub.6 is hydrogen or a lower alkyl group having 1 to 3 carbon atoms and n is 3, 4 or 5. A method for percutaneously administering such a composition is also disclosed.

Abstract: Bioerodible ortho ester polymers useful for preparing bioerodible pharmaceutical compositions such as implants, ointments, creams, gels and the like are provided. The pharmaceutical compositions of the invention are useful for the controlled release of therapeutic agents, and may be administered for a variety of purposes, such as for the treatment of deep wounds, including burns, and for the treatment of periodontal disease.

Abstract: A method of percutaneously administering a physiologically active agent which comprises applying to the skin of a mammal a physiologically active agent in a carrier system which comprises at least one adjuvant, at least one solvent and at least one diol and/or triol moderator. The adjuvant can be selected from aliphatic hydrocarbons, halogen substituted aliphatic hydrocarbons, alcohol esters of aliphatic carboxylic acids, mono- or di-ethers, ketones, higher monoalcohols or mixtures thereof. The solvent can be selected from thioglycerols, lactic acid and esters thereof, cyclic ureas, compounds represented by the general formula R.sub.1 R.sub.2 NCONR.sub.3 R.sub.4, pyrrolidone-type compounds, amides, lactones or mixtures thereof.

Abstract: A family of composites suitable for use as materials of construction for implantable medical devices is disclosed. In the most preferred embodiment, the substrate polymer is an ortho ester polymer formed by the reaction of a ketene acetal having a functionality of two or more with a polyol. Also in the most preferred embodiment, the reinforcement material in the composites is calcium-sodium metaphosphate ("CSM") fibers. In other embodiments, the composites may replace either (but not both) of the substrate or the reinforcement with materials of the art.

Abstract: Bioerodible ortho ester polymers useful for preparing soft form bioerodible pharmaceutical compositions such as ointments, creams, gels and the like are provided. A novel synthetic method for preparing the polymers is provided as well. Synthesis involves a one-step reaction between a monomeric ortho ester and a triol. The pharmaceutical compositions of the invention are useful for the controlled release of therapeutic agents, and may be administered for a variety of purposes, such as for the treatment of deep wounds, including burns, and for the treatment of periodontal disease.

Abstract: Transdermal drug delivery systems comprise a backing or enclosure having a matrix layer which incorporates a drug and a percutaneous enhancer for the drug. The percutaneous enhancer and/or drug will be contained within polymeric particles dispersed through the matrix layer, where the polymeric particles define pore networks which are sized to release the enhancer and/or drug into the matrix layer at rate(s) selected to provide for a desired rate of drug penetration. By isolating the enhancer within the polymeric particles, adverse interactions between the enhancer and the matrix layer and/or the drug can be minimized. Moreover, the release rate of the enhancer into the matrix layer can be carefully controlled, which in turn controls the penetration rate of the drug into the treated host.

Abstract: Biodegradable ortho ester polymers based on mono- and poly-thiols are provided that are useful for making biodegradable sustained release agent dispensers and which contain at least one of the mer units (I), (II), (III) or (IV) ##STR1## wherein X is a quadrivalent organic grouping, A and B are independently selected from the group consisting of hydrogen and lower alkyl, and R is hydrocarbyl or oxyhydrocarbyl of 1 to 14 carbon atoms, if oxyhydrocarbyl, containing 1 to 4 oxy groups, and may be either aliphatic or aryl, unsubstituted or substituted with one or more lower alkyl, amino, nitro or halogen moieties.

Abstract: Biodegradable polymers that are useful for making biodegradable sustained release agent dispensers and which contain acetal, carboxy-acetal, ortho ester and/or carboxy-ortho ester linkages.

Abstract: Polymers are provided that are useful for making biodegradable sustained release agent dispensers and which contain at least one of the following mer units (I) and (II) ##STR1## wherein X is a quadrivalent organic grouping, A and B are hydrogen or lower alkyl, and R is hydrocarbyl or oxyhydrocarbyl of 1 to 14 carbon atoms and, if oxyhydrocarbyl, containing 1 to 4 oxy groups, and may be either aliphatic or aryl, unsubstituted or substituted with one or more lower alkyl, amino, nitro or halogen moieties. Methods of synthesizing the novel polymers are also provided, as biodegradable beneficial agent dispensers prepared using the novel polymers.

Abstract: Water-soluble polyacetal or polyketal having the formula ##STR1## wherein R.sub.1, and R.sub.2 are aliphatic, cycloaliphatic or aromatic groups, for ketals; R.sub.1 is hydrogen and R.sub.2 is aliphatic, cycloaliphatic, or aromatic groups for acetals; R.sub.3 and R.sub.4 are also aliphatic, alkoxy, cycloaliphatic or aromatic groups X represents groups as (CH.sub.2).sub.n, O(CH.sub.2).sub.N O or ##STR2## that connect the pendant unsaturation to the aliphatic, cycloaliphatic or aromatic R.sup.4 groups, the ratio of a to b is 0.5 to 10, and n is 10-100.

Abstract: Biodegradible polymers are provided which may contain a biologically active substance, e.g. a drug such as insulin, which is released over a period of time as the polymer erodes when in contact with a body fluid. The polymer contains an amine functionality whereby it erodes faster at low acid pH's than at higher acid pH's. As an example, the polymer may contain insulin and may contain or may have an encapsulating hydrogel containing glucose oxidase. As the blood sugar level of a diabetic person rises, e.g., after a meal, glucose diffuses into the polymer or hydrogel and is converted to gluconic acid which lowers the pH, and accelerates erosion and the release of insulin.

Abstract: A therapeutic composition comprising a therapeutic macromolecular agent incorporated in cross-linked polyacetal.

Abstract: The instant invention is directed to a polymer with at least one labile backbone bond per repeat unit and at least one pendant acid functionality per thousand repeat units.The instant invention is also directed to a controlled release device which comprises:(A) a polymer with at least one labile backbone bond per repeat unit and at least one pendant acid functionality per thousand repeat units; and(B) a beneficial substance incorporated within or surrounded by the matrix of said polymer.

Abstract: Biodegradible polymers are provided which may contain a biologically active substance, e.g. a drug such as insulin, which is released over a period of time as the polymer erodes when in contact with a body fluid. The polymer contains an amine functionality whereby it erodes faster at low acid pH's than at higher acid pH's. As an example, the polymer may contain insulin and may contain or may have an encapsulating hydrogel containing glucose oxidase. As the blood sugar level of a diabetic person rises, e.g., afte a meal, glucose diffuses into the polymer or hydrogel and is converted to gluconic acid which lowers the pH, and accelerates erosion and the release of insulin.

Abstract: A method of percutaneously administering a physiologically active agent which comprises applying to the skin of a mammal a physiologically active agent in a carrier system which comprises at least one adjuvant and at least one solvent. The adjuvant can be selected from higher monoalcohols or mixtures thereof. The solvent can be selected from thioglycerols, lactic acid and esters thereof, cyclic ureas, compounds represented by the general formula R.sub.1 R.sub.2 NCONR.sub.3 R.sub.4, pyrrolidone-type compounds, amides, lactones or mixtures thereof.